Murine anti-tumor activity of new water soluble platinum(II) complexes with reduced toxicity.
A series of new water soluble sugar and non-sugar containing platinum(II) complexes was synthesized and evaluated for effects of the sugar moiety on water solubility, anti-tumor activity, and acute leukopenia. When tested in vivo against the murine P388 and L1210 leukemias at LD10/maximally effective doses, the compound cis-[(gluconylamino)malonato-O,O'](1R,2R-cyclohexanediami ne-N,N')platinum (II), R,RG-AMP produced comparable or superior anti-tumor activity to cisplatin, carboplatin, and tetraplatin. Efficacy was also demonstrated for the L1210/DDP (cisplatin-resistant) leukemia. Further, R,R-G-AMP is non-nephrotoxic and produces less leukopenia than cisplatin, carboplatin, and tetraplatin.
Talebian
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AH
Department of Chemistry, Georgetown University, Washington, DC 20057.
Bensely
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Schein
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Green
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D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity*; D001853:Bone Marrow / Q000187:drug effects; D002241:Carbohydrates / Q000494:pharmacology; D007668:Kidney / Q000187:drug effects; D051379:Mice; D009944:Organoplatinum Compounds / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity*; D012995:Solubility; D014867:Water
D000970:Antineoplastic Agents; D002241:Carbohydrates; D009944:Organoplatinum Compounds; D014867:Water